1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Bepotastine tosylate

Bepotastine tosylate 

Cat. No.: HY-I0021A
Handling Instructions

Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate can suppress the expression of nerve growth factor (NGF). Bepotastine tosylate can be used in studies of allergic rhinitis, allergic conjunctivitis and urticaria/pruritus.

For research use only. We do not sell to patients.

Bepotastine tosylate Chemical Structure

Bepotastine tosylate Chemical Structure

CAS No. : 1160415-45-1

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Description

Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate can suppress the expression of nerve growth factor (NGF). Bepotastine tosylate can be used in studies of allergic rhinitis, allergic conjunctivitis and urticaria/pruritus[1][2][3][4].

IC50 & Target

Histamine H1 Receptor[1][2][3][4].

In Vitro

Bepotastine tosylate (10, 100, 1000 µM; preincubates for 120 min) decreases the release of histamine induced by A23187 treatment, which reaches a statistically significant reduces level at 1000 µM[1].
Bepotastine tosylate (50 µM; 1 h) suppresses the expression of NGF mRNA in NHEKs[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: RPMCs
Concentration: 10, 100, 1000 µM
Incubation Time: 120 min (preincubate)
Result: Decreased the release of histamine.

Western Blot Analysis[2]

Cell Line: NHEKs
Concentration: 50 µM (preincubation)
Incubation Time: 1 h
Result: Suppressed the expression of NGF mRNA in NHEKs.
In Vivo

Bepotastine tosylate (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of PAF-induced conjunctival eosinophil infiltration[1].
Bepotastine tosylate (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, which are almost the same levels compares with the control[3].
Bepotastine tosylate (10 mg/kg; p.o.; once) significantly suppresses serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Guinea pigs (6-week-old)[1].
Dosage: 10 g/L (1.0% (w/v)) for 10 µL.
Administration: Eye drop; 3 times at intervals of 20 min (in one eye)
Result: Inhibited PAF-induced conjunctival eosinophil infiltration.
Animal Model: Male BALB/c mice(12-week-old); NC/Nga mice[3].
Dosage: 3, 10 mg/kg
Administration: Oral administration; once (1 h before induces scratching behavior of Male BALB/c mice).
Result: Significantly inhibited histamine-mediated scratching behavior in male BALB/c mice.
Significantly suppressed serum LTB 4 levels in NC/Nga mice with a rash.
Molecular Weight

561.09

Formula

C28H33ClN2O6S

CAS No.
SMILES

O=S(C1=CC=C(C)C=C1)(O)=O.O=C(O)CCCN2CCC(CC2)O[[email protected]](C3=NC=CC=C3)C(C=C4)=CC=C4Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Bepotastine tosylate
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